XAV-939

目录号:S1180 别名: NVP-XAV939

XAV-939 Chemical Structure

Molecular Weight(MW): 312.31

XAV-939通过抑制tankyrase1/2而选择性抑制Wnt/β-catenin介导的转录,无细胞试验中IC50为11 nM/4 nM,调节轴蛋白水平,而对 CRE, NF-κB和TGF-β无作用。

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客户使用该产品的7个实验数据:

  • Fluorescence microscopy of pSuper or Cdo shRNA expressing P19 cells at ITS1 immunostained withβ-tubulin III antibodies. Size bar=100 um. P19/control or P19/Cdo shRNA cells were treated with DMSO or XAV939 in the differentiation medium for 72 h followed by immunostaining.

    Nat Commun 2014 5, 5455. XAV-939 purchased from Selleck.

    (I) Effect of XAV-939 on gefitinib efficacy in indicated NSCLC cells was detected by MTT assay (J) The indicated NSCLC cells were treated with gefitinib in the presence or absence of XAV-939, and then subjected to immunoblot analysis using the indicated antibodies. Data represent the mean ± SD of three independent experiments. *P < 0.05.

    Cancer Lett, 2017, 400:194-202. XAV-939 purchased from Selleck.

  • Images of the hfVM experiment described in C, comparing the effects of LIF-nano versus empty-nano at equivalent dilution (left panel) and XAV-nano versus empty-nano at equivalent dilution (right panel). Scale bars: 200 μm.

    Dis Model Mech 2014 7(10), 1193-203. XAV-939 purchased from Selleck.

    Pathology observation of mice liver sections stained with hematoxylin and eosin (H&E) and Masson (×200), and the levels of -SMA and Tmem88 were analyzed by immunohistochemistry (×200).

    Mol Immunol, 2016, 80:58-67. XAV-939 purchased from Selleck.

  • Cells plated at 2 x 104 in 24 multiwell with DMEM 10% FBS preconditioning 24 hrs (pretreatment without wnt) switch medium from 2% HS + WNT 100 ng/ml

    Dr. Marco Quarta of Stanford University. XAV-939 purchased from Selleck.

     

    Fig. 1.  Canonical Wnt Signaling Inhibits Prostatic Bud Number Similar to TCDD. E14.5 male UGSs were cultured for 4 days in media containing 10 nM DHT with either vehicle 1 nM TCDD; recombinant DKK1 + DKK2 (500 ng/ml each); or 10 μM XAV-939 to inhibit canonical Wnt signaling. Buds were visualized by performing IHC specific for ecadherin, an epithelium marker (green).  The number of prostatic buds was determined by confocal microscopy. Yellow arrowheads indicate areas where buds are present. U indicates urethra.  Results are mean ±SE for at least four litter-independent samples per treatment. Asterisk indicates a significant decrease compared to control p < 0.05.

    XAV-939 purchased from Selleck.

  • XAV-939 purchased from Selleck.

产品安全说明书

Wnt/beta-catenin抑制剂选择性比较

生物活性

产品描述 XAV-939通过抑制tankyrase1/2而选择性抑制Wnt/β-catenin介导的转录,无细胞试验中IC50为11 nM/4 nM,调节轴蛋白水平,而对 CRE, NF-κB和TGF-β无作用。
靶点
TNKS2 [1]
(Cell-free assay)
TNKS1 [1]
(Cell-free assay)
4 nM 11 nM
体外研究

XAV939 是小分子选择性抑制剂,抑制Wnt通路转录因子β-catenin调节的转录,作用于TNKS1和TNKS2时IC50分别为11和4nM。XAV939通过稳定axin和断裂混合物的极限浓度组成促进β-catenin降解, 而稳定axin是通过阻断PAR酶:端锚聚合酶1和2 。2种端锚聚合酶亚型因为axin的高度保守区而相互作用,促进了端锚聚合酶通过泛素-蛋白酶体途径的降解。XAV939抑制Wnt/β-catenin通路活性已经用于多种癌症治疗。[1] XAV939尤其抑制端锚聚合酶PARP活性。XAV939 明显降低DNA-PKcs蛋白水平, 说明了在维持DNA-PKcs蛋白稳定性时端锚聚合酶PARP活性的关键性。用1.0 μM XAV939处理12小时,DNA-PKcs蛋白水平降低到最低水平,与用DMSO处理的对照组相比,相对表达量小于25%。1.0 μM XAV939治疗人类成淋巴细胞,导致端锚聚合酶1水平明显上升。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf-21 MUPLbY5ie2ViQYPzZZk> NVTQUFQ6OThwN{Wg{txO M1PQUVYxKG2rbh?= MWfEUXNQ NHnBTJJKdmirYnn0bY9vKG:oIF6teIVzdWmwYXygS3NVNXSjZ3fl[EBVVkuVMjDlfJBz\XO|ZXSge4l1cCCLQ{WwJI9nKDBwMEC1N{DPxE1? NEjURpIzOzh5OUSzNS=>
HEK293T NHPKc4FHfW6ldHnvckBCe3OjeR?= MmK0SG1UVw>? MYLJcohq[mm2aX;uJI9nKFewdDDzbYdv[WyrbnegZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDmc5J{c2:uaX6tbY5lfWOnZDDjRW1RKHKnc4DvcpNmKGWuZX3lcpQh[WO2aY\heIlwdiC5aYToJGlEPTBib3[gNE4xPzhizszN NWrjWZRvOjN6N{m0N|E>
HEK293T NIDLW49HfW6ldHnvckBCe3OjeR?= M4\2SFExKM7:TR?= NVX6fIZkTE2VTx?= NGjKWpVKdmirYnn0bY9vKG:oIHLleIEu[2G|ZXnuMYRmeGWwZHXueEBk[W6xbnnjZYwhX262MzDwZZRpf2G7IIfpeIghUUN3MDDv[kAxNjB3MTFOwG0> MmTPNlIyQTF3NUe=
HEK293T NXL0W3VvTnWwY4Tpc44hSXO|YYm= MkDpNlQhcA>? MX3EUXNQ NEDJPHdKdmirYnn0bY9vKG:oIH3veZNmKFewdEPBJJNq\26jbHnu[{B4cXSqIFnDOVAhd2ZiMD6wO|gh|ryP NHq2ZpQzOjJ4MEKwNy=>
SW480 M13TTmZ2dmO2aX;uJGF{e2G7 NXn4THM4OTBizszN Mo\XNlQhcA>? M13kVWROW09? MljVV5Ri[mmuaYrheIlwdiCxZjDBfIlvOiC5aYToJGVEPTBib3[gNE4{PzFizszN MX:yNlI3ODJyMx?=
HEK293T M1Gw[mZ2dmO2aX;uJGF{e2G7 MkjUOVAh|ryP MlLhSG1UVw>? MYHIZZMhdm9iRX\m[YN1KG:wIH\vdpNsd2yrbj3pcoR2[2WmIHPBUXAhe2mpbnHsbY5oKGmwIHj1cYFvKEiHS{K5N3Qh[2WubIOgZ49mgHC{ZYPzbY5oKEOURR?= MV:yNlI3ODJyMx?=
IEC-6 Mk\6SpVv[3Srb36gRZN{[Xl? NUezXoY5PiCq MmXtRY51[WexbnnzeEBi[3Srdnn0fUBifCCEZYThMYNifGWwaX6vWGNHKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhX262LUPhMYlv\HWlZXSgZZhqdjJiZYjwdoV{e2mxbjD3bZRpKEmFNUCgc4YhOC54NDFOwG0> NUP1cVY6OjRyNkC0PFk>
IEC-6 MVjGeY5kfGmxbjDBd5NigQ>? MXS2JIg> MYfBcpRi\2:waYP0JIFkfGm4aYT5JIF1KEKndHGtZ4F1\W6rbj;UR2Yh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBYdnRvM3GtbY5lfWOnZDDs[5I2KGW6cILld5Nqd25id3n0bEBKSzVyIH;mJFIvQSEQvF2= NULXdHNyOjRyNkC0PFk>
DLD1 MlrESpVv[3Srb36gRZN{[Xl? NVHKVYVbOjBizszN MoftNlQhcA>? NFjON|ZFVVOR NVHYT4lUUW6qaXLpeIlwdiCxZjD0ZY5sgXKjc3WgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDUR2Yu\GWyZX7k[Y51KHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fS=> NXr5WIxjOjR3Mke3PVI>
DLD1 NEfTfpdEgXSxdH;4bYMhSXO|YYm= NVPKU|hSOjBizszN NWnoZZlFOTBiZB?= MUHEUXNQ M3j2XWN6fG:2b4jpZ4l1gSCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbh?= MlS1NlQ2Ojd5OUK=
VERO MlOzSpVv[3Srb36gRZN{[Xl? MXuyOUDPxE1? MUjEUXNQ NIjq[HdFcXO2dYLi[ZMhWEGUIHLlcJQhe3mwdHjld4l{NCCjZn\lZ5RqdmdidHjlJIFkfGmwIHP5eI9{c2WuZYTvckwh[2WubDDzbIFx\SCjbnSgZ4VtdCCjZHjld4lwdg>? NHrBbXEzPTN|Mki0OS=>
HeLa M3HGUWZ2dmO2aX;uJGF{e2G7 Mn3ZNVAh|ryP NXjjfJRlPDhiaB?= MojaVoVlfWO2aX;uJI9nKGO7dH;wcIF{dWmlIHTpd5RzcWK3dHnvckBidmRiboXjcIVieiC2cnHud4xw[2G2aX;uJI9nKM7{LXPheIVvcW5? MoPuNlUxPjF2OUm=
SiHa NVLrW5pmTnWwY4Tpc44hSXO|YYm= NHPnS3oyOCEQvF2= NX:1cmNiPDhiaB?= MlfuVoVlfWO2aX;uJI9nKGO7dH;wcIF{dWmlIHTpd5RzcWK3dHnvckBidmRiboXjcIVieiC2cnHud4xw[2G2aX;uJI9nKM7{LXPheIVvcW5? NFjKOIQzPTB4MUS5PS=>

... Click to View More Cell Line Experimental Data

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[2]
+ 展开
  • Cell lines: WTK1成淋巴细胞
  • Concentrations: 1.0 μM
  • Incubation Time: 8小时
  • Method: XAV939溶解在DMSO中,储存浓度为10mM, 实验处理时稀释到100 μM。实验组,用1.0 μM XAV939处理WTK1成淋巴细胞8小时,对照组用DMSO处理,上样到4-20%梯度SDS-PAGE孔中。2小时上样一次。在0, 2,和4 小时分别上样,结果分别跑胶2, 4,和6小时。最后,通过western blot分析。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 12 mg/mL (38.42 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+corn oil
1mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 312.31
化学式

C14H11F3N2OS

CAS号 284028-89-3
稳定性 powder
in solvent
别名 NVP-XAV939

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    I want to inject XAV 939 (Cat # S1180) into mice through I.P. and just wonder what kind of solvent/solution I can use for this.

  • 回答:

    S1180 XAV-939 can be dissolved in 4% DMSO+corn oil at 1 mg/ml as a clear solution. When preparing the solution, please dissolve the compound in DMSO clearly first. You can sonicate and warm it in water bath at about 45 degree to help dissolving. Then dilute with corn oil.

Wnt/beta-catenin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID